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Estraimod Immediate Release

Phase 1

Healthy Participants | Small molecule | Other |Pfizer, Inc.|Last Updated: Feb 10, 2025

Success Probability
Approval Probability 71%
TA Base Rate26%
Adjusted LOA41%
ML RiskLOW_RISK
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Market & Valuation
rNPV $3.2B
Market Size $9.4B
Revenue Basis $1.6B
Competitors 6
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Trial Design
RandomizedCONTROLLEDBiomarker
Total Trials1
Total Enrollment16
FDA Designations
No designations recorded
Clinical Trials (1)
NCT IDTitlePhaseStatusEnrollmentVelocityDesignStartCompletionLast UpdatedSitesCountries
NCT05956002A Study to Evaluate the Study Medication (Etrasimod) When Mixed With Food in Healthy ParticipantsPHASE1 COMPLETED 16Sep 4, 2023Jan 4, 2024Feb 10, 20251 Belgium
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Study Endpoints
Primary Endpoints
Area Under the Plasma Concentration-Time Curve From Time Zero to the Time of the Last Quantifiable Concentration (AUClast) of Etrasimod
At pre-dose and 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Day 1 of each period

AUClast was calculated using linear/log trapezoidal method.

Area Under the Concentration-time Curve From Time Zero Extrapolated to Infinity (AUCinf) of Etrasimod
At pre-dose and 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Day 1 of each period

AUCinf was calculated as AUClast + (Clast\*/kel), where Clast is the predicted plasma concentration at the last quantifiable time point from the log-linear regression analysis, and kel is the terminal phase rate constant calculated by a linear regression of the loglinear concentration-time curve.

Maximum Observed Plasma Concentration (Cmax) for Etrasimod
At pre-dose and 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Day 1 of each period
Secondary Endpoints
Change From Baseline in Heart Rate at 1, 2, 3, 4, 5, 6, 8 and 24 Hours on Day 1
Baseline, 1, 2, 3, 4, 5, 6, 8 and 24 hours post dose on Day 1
Number of Participants With Treatment Emergent Adverse Events (TEAEs)
From start of study treatment up to 28-35 days after last dose of study treatment (maximum up to 72 days)
Number of Participants With Clinical Laboratory Abnormalities
Up to Day 45
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Study Design & Arms
AllocationRANDOMIZED
MaskingNONE
ModelCROSSOVER
PurposeBASIC_SCIENCE
Treatment Arms
ArmTypeDescription
Sequence 1EXPERIMENTALSingle oral dose of etrasimod 2 mg clinical IR tablet under fasted conditions (Reference) followed by single oral dose of etrasimod 2 mg mini tablets mixed with applesauce under fasted conditions (Test 1) followed by single oral dose of etrasimod 2 mg mini tablets mixed with chocolate pudding under fasted conditions (Test 2) followed by single oral dose of etrasimod 2 mg mini tablets mixed with water under fasted conditions (Test 3) followed by single oral dose of etrasimod 2 mg mini tablets mixed with yogurt under fasted conditions (Test 4)
Sequence 2EXPERIMENTALSingle oral dose of etrasimod 2 mg mini tablets mixed with applesauce under fasted conditions (Test 1) followed by single oral dose of etrasimod 2 mg mini tablets mixed with water under fasted conditions (Test 3) followed by single oral dose of etrasimod 2 mg clinical IR tablet under fasted conditions (Reference) followed by single oral dose of etrasimod 2 mg mini tablets mixed with chocolate pudding under fasted conditions (Test 2) followed by single oral dose of etrasimod 2 mg mini tablets mixed with yogurt under fasted conditions (Test 4)
Sequence 3EXPERIMENTALSingle oral dose of etrasimod 2 mg mini tablets mixed with chocolate pudding under fasted conditions (Test 2). Followed by single oral dose of etrasimod 2 mg clinical IR tablet under fasted conditions (Reference).followed by single oral dose of etrasimod 2 mg mini tablets mixed with water under fasted conditions (Test 3). Followed by single oral dose of etrasimod 2 mg mini tablets mixed with applesauce under fasted conditions (Test 1) Followed by single oral dose of etrasimod 2 mg mini tablets mixed with yogurt under fasted conditions (Test 4)
Sequence 4EXPERIMENTALSingle oral dose of etrasimod 2 mg mini tablets mixed with water under fasted conditions (Test 3). Followed by single oral dose of etrasimod 2 mg mini tablets mixed with chocolate pudding under fasted conditions (Test 2). Followed by single oral dose of etrasimod 2 mg mini tablets mixed with applesauce under fasted conditions (Test 1). Followed by single oral dose of etrasimod 2 mg clinical IR tablet under fasted conditions (Reference). Followed by single oral dose of etrasimod 2 mg mini tablets mixed with yogurt under fasted conditions (Test 4)
Interventions
NameTypeDescription
Estraimod Immediate Release (IR)DRUGan immediate release tablet
Etrasimod Mini Tab in waterDRUGvery small tablet mixed in water
Etrasimod Mini Tab in chocolate puddingDRUGvery small tablet mixed in chocolate pudding
Etrasimod Mini Tab in yogurtDRUGVery small tablet mixed in yogurt
Etrasimod Mini Tab in applesauceDRUGVery small tablet mixed in applesauce
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Eligibility Criteria
Age Range18 Years — N/A
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * Healthy participants * BMI 16 to 32 kg/m2 * body weight more than 50kg Exclusion Criteria: * Ongoing or past history of significant medical conditions * Eye disorders such as macular edema or uveitis * Ongoing or recent infections * Use of prescription or non prescription me...

Countries:Belgium
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